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以6-氨基青霉烷酸为原料，经10步反应合成了他唑巴坦钠。6－APA经重氮化、溴化转变为6α－溴代青霉烷酸（1），在二苯腙存在下用过氧醋酸氧化一步生成6－α溴代青霉亚砜酸二苯甲酯（2），再以锌粉还原得6，6-二氢青霉亚砜酸二苯甲酯（3），（3）与2-巯基苯骈噻唑共热得氮杂环丁酮二硫化物（4），（4）用无水氯化铜反应得2β-氯甲基青霉烷酸二苯甲酯（5），（5）在DMF中与叠氮化钠作用得混合物（6），（6）以高锰酸钾氧化后生成物用分级结晶分离出2β-叠氮甲基青霉砜酸二苯甲酯（7a），后者与乙炔环加成生成他唑巴坦二苯甲酯（8），接着用间-甲酚脱羧基保护基而得到他唑巴坦（9），最后以异辛酸钠成盐处理而得目的物（10）他唑巴坦钠。
Tazobactam sodium was synthesized by 10 steps using 6-aminopenicillanic acid as raw material. 6-APA diazotization, bromination into 6α-bromo penicillanic acid (1), in the presence of diphenylhydrazone generated by oxidation of peracetic acid 6-α-bromoperoxide bromoxime Ester (2), and then reduced to zinc powder 6,6-dihydro-penicillin sulfoxide acid diphenylmethyl ester (3), (3) and 2-mercaptobenzothiazole were heated in azetidine disulfide (4) Reaction of 2β-chloromethyl penicillanic acid diphenylmethyl ester (5) with anhydrous copper chloride, (5) Reaction with sodium azide in DMF to obtain a mixture (6) , (6) After oxidation with potassium permanganate The product is separated by fractional crystallization from diphenylmethyl 2β-azidomethyl penicillanate (7a), which is coupled with an acetylene ring to form tazobactam diphenyl (8) followed by decarboxylation with m-cresol to give tazobactam (9), and finally sodium salt of isooctanoate to give the desired product (10) tazobactam sodium.